Dextropropoxyphene was first patented in 1955 and subsequently manufactured by Eli Lilly and Company.[citation needed]

Due to its euphoric and analgesic effects, dextropropoxyphene is known to be habit forming, albeit not to the same extent as other opioids such as morphine or heroin.[citation needed]Notably, dextropropoxyphene is also known to cause seizures and potentially fatal cardiac arrhythmia at high doses[citation needed], which are not able to be reversed by naloxone.[citation needed]

Today, dextropropoxyphene is rarely encountered on the streets and is sometimes obtained by prescription from a compounding pharmacy.[citation needed] It is strongly recommended that one research this substance's toxicity and use proper harm reduction practices if choosing to use this substance.

Chemistry

Dextropropoxyphene is similar in structure to tapentadol. While tapentadol has an ethyl substitution on the gamma-carbon, dextropropoxyphene instead has both benzyl and propionyl substitutions. Dextropropoxyphene also contains a benzene ring in place of the phenol ring found in tapentadol. The empirical formula of dextropropoxyphene is C22H29NO2 and has a molar mass of 339.471 grams per mole.

Pharmacology

Opioids produce their effects by binding to and activating the μ-opioidreceptor. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.

Unlike most opioids, dextropropoxyphene is also a weak serotoninreuptake inhibitor as well as a potent nicotinic acetylcholine antagonist[2]. Dextropropoxyphene has a bioavailability of about 40% and is metabolized by the cytochrome P450 3A4 enzyme. The optical isomer of dextropropoxyphene, levopropoxyphene has no analgesic activity but retains antitussive effects.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWikicontributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects

The general sensation of dextropropoxyphene can be described as one of euphoria, relaxation, anxiety suppression and pain relief.

Physical euphoria - This particular substance can be considered as less intense in its physical euphoria when compared with that of morphine or diacetylmorphine (heroin). The sensation itself can be described as extreme feelings of intense physical comfort, warmth, love and bliss.

Respiratory depression - At low to moderate doses, this effect results in the sensation that the breath is slowed down mildly to moderately, but does not cause noticeable impairment. At high doses and overdoses, opioid-induced respiratory depression can result in a shortness of breath, abnormal breathing patterns, semi-consciousness, or unconsciousness. Severe overdoses can result in a coma or death without immediate medical attention.

Cognitive effects

Cognitive euphoria - This particular substance can be considered as less intense in its cognitive euphoria when compared with that of morphine or diacetylmorphine (heroin). The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness.

Experience reports

Toxicity and harm potential

Dextropropoxyphene has a high toxicity relative to dose. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. It is also potentially lethal when mixed with depressants like alcohol or benzodiazepines and generally has a wider range of substances which it is dangerous to combine with in comparison to other opioids. Dextropropoxyphene is known to lower the seizure threshold. It should not be taken during benzodiazepine withdrawals as this can potentially cause seizures. Dextropropoxyphene is known to cause potentially fatal heart arrhythmias, and it is discouraged to take in very heavy doses or several days in a row.

Tolerance and addiction potential

As with other opioids, the chronic use of dextropropoxyphene can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of dextropropoxyphene develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Dextropropoxyphene presents cross-tolerance with all other opioids, meaning that after the consumption of dextropropoxyphene all opioids will have a reduced effect.

Dangerous interactions

Although many psychoactive substances are reasonably safe to use on their own, they can quickly become harmful and even life-threatening when taken with other substances. The following section lists some known dangerous combinations, but it may not include all of them. Furthermore, a combination that seems to be harmless in low doses can still greatly increase the risk of injury or death when the doses are slightly increased. Independent research should always be conducted to ensure that a combination of two or more substances is safe to consume. Some interactions listed have been sourced from Tripsit.

Stimulants - It can be dangerous to combine depressants with stimulants due to the risk of accidental excessive intoxication. Stimulants mask the sedative effect of depressants, which is the main factor most people use to gauge their level of intoxication. Once the stimulant effects wear off, the effects of the depressant will significantly increase, leading to intensified disinhibition, motor control loss, and dangerous black-out states. This combination can also potentially result in severe dehydration if one's fluid intake is not closely monitored. If choosing to combine these substances, one should strictly limit themselves to a pre-set schedule of dosing only a certain amount per hour until a maximum threshold has been reached.

Serotonin-norepinephrine reuptake inhibitors (SNRIs) such as tramadol and DXM

5-HTP

Legality

United States - Dextropropoxyphene is a Schedule II or Schedule IV Controlled Substance depending on the dosage and other ingredients.[4] Dextropropoxyphene has been withdrawn in the United States and is no longer available through prescription, although it is possible some compounding pharmacies may still carry it.

United Kingdom - Dextropropoxyphene is a Class C, Schedule 2 or Schedule 5 substance depending on the dose.[5]